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作 者:赵利刚[1] 李燕[2] 吕立勋[1] 赵琳琳[1]
机构地区:[1]河北联合大学药学院,河北唐山063000 [2]唐山市妇幼保健院药剂科,河北唐山063000
出 处:《中国医药工业杂志》2014年第5期444-448,共5页Chinese Journal of Pharmaceuticals
基 金:河北省自然科学基金石药联合基金"α-萜品醇脂肪酸酯类衍生物经皮促透作用的可逆性及其机理研究"(H2013209098)
摘 要:制备了含不同促透剂[月桂氮酮、油酸、N-甲基吡咯烷酮(NMP)、薄荷醇、庚酸薄荷醇酯(M-HEP)或油酸薄荷醇酯(M-OA)]的盐酸司来吉兰压敏胶分散型贴剂。采用双室扩散池,以离体大鼠皮肤为屏障进行体外渗透试验,考察了压敏胶和促透剂的种类及浓度对贴剂中药物渗透行为的影响。结果表明,以丙烯酸树脂压敏胶Duro-Tak 87-2677为基质,3%薄荷醇与10%月桂氮酮联用时贴剂中盐酸司来吉兰的累积透过量较高且无释放时滞。初步稳定性考察结果表明,该制品在30℃、相对湿度60%环境放置6月,黏附性和透皮性能无显著改变。The drug-in-adhesive patches loaded with selegiline hydrochloride with azone, oleic acid, N-methylpy rrolidone (NMP), menthol, 2-isopropyl-5-methylcyclohexyl heptanoate (M-HEP) or (E) -2-isopropyl-5-methylcyclohexyl octadec-9-enoate (M-OA) as penetration enhancer were prepared, respectively. The in vitro permeability test was carried out with two-chamber cells and excised rat skin to investigate the effects of the types and concentrations of pressure sensitive adhesive (PSA) and enhancer on permeation behavior of the drug in patches. The results showed that the optimal patches with Duro-Tak 87-2677 as the matrix, 3 % menthol and 10 % azone as combined enhancers had a higher penetration amount and no time lag in release. The results of preliminary stability test showed that the adhesion and in vitro transdermal property of the product stored at 30 ℃ and relative humidity of 60% for 6 months had no significant changes.
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